1451055-94-9Relevant academic research and scientific papers
C - 2 bit and C - 4 of the modified 1 - deoxy taxane compound and its preparation method
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Paragraph 0056, (2018/10/19)
The invention relates to a C - 2 bit and C - 4 of the modified 1 - deoxy taxane compound and its preparation method. The structure of the compound is: Wherein in the formula R1 Solidification butoxy or amyl; R2 To a two methoxy acyl or [...] benzoyl; R3 For the cyclopropanecarboxylic formyl. The invention of 1 - deoxy taxane compounds in the C - 2 members will be benzoyl adapted for the meta-substituted benzoyl and C - 4 introduces cyclopropanecarboxylic formyl, retention of the taxane ring skeleton and the necessary functional group, enriches the compounds, through original screening experiment, activity experiment and other related data show that the partial compound in cell toxicity in good than the taxol, at the same time also for this kind of compound activity relationship study provides valuable reference.
Synthesis and antitumor activity of 1-deoxybaccatin III analogs from 1-deoxybaccatin VI
Qiu, Yuan-You,Lin, Hai-Xia,Cui, Yong-Mei,Shao, Jun-Chao,Jin, Dan-Hui
, p. 1573 - 1582 (2013/10/22)
Several new 1-deoxybaccatin III analogs were conveniently synthesized from 1-deoxybaccatin VI with the aim of having modified ester groups at C-2 and C-4. The antitumor activity of these compounds was evaluated. The preliminary SAR analysis showed that the electronic properties of the terminal group in the substituent on C4, C9, and C10 constituted important factors to the cytotoxic activities against A 549 and MCF-7 cell lines. The present studies provide a new synthetic basis for development of new 1-deoxypaclitaxel analogs. Graphical Abstract: [Figure not available: see fulltext.].
